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Page 1
Design, synthesis and structure activity relationships of indazole and indole derivatives as potent glucagon receptor antagonists.
Song F, Xu G, Gaul MD, Zhao B, Lu T, Zhang R, DesJarlais RL, DiLoreto K, Huebert N, Shook B, Rentzeperis D, Santulli R, Eckardt A, Demarest K. Song F, et al. Among authors: desjarlais rl. Bioorg Med Chem Lett. 2019 Aug 1;29(15):1974-1980. doi: 10.1016/j.bmcl.2019.05.036. Epub 2019 May 18. Bioorg Med Chem Lett. 2019. PMID: 31138472
Discovery of Potent and Orally Bioavailable Pyridine N-Oxide-Based Factor XIa Inhibitors through Exploiting Nonclassical Interactions.
Xu G, Liu Z, Wang X, Lu T, DesJarlais RL, Thieu T, Zhang J, Devine ZH, Du F, Li Q, Milligan CM, Shaffer P, Cedervall PE, Spurlino JC, Stratton CF, Pietrak B, Szewczuk LM, Wong V, Steele RA, Bruinzeel W, Chintala M, Silva J, Gaul MD, Macielag MJ, Nargund R. Xu G, et al. Among authors: desjarlais rl. J Med Chem. 2022 Aug 11;65(15):10419-10440. doi: 10.1021/acs.jmedchem.2c00442. Epub 2022 Jul 21. J Med Chem. 2022. PMID: 35862732
6-Benzhydryl-4-amino-quinolin-2-ones as Potent Cannabinoid Type 1 (CB1) Receptor Inverse Agonists and Chemical Modifications for Peripheral Selectivity.
Zhang YM, Greco MN, Macielag MJ, Teleha CA, DesJarlais RL, Tang Y, Ho G, Hou C, Chen C, Zhao S, Kauffman J, Camacho R, Qi J, Murray W, Demarest K, Leonard J. Zhang YM, et al. Among authors: desjarlais rl. J Med Chem. 2018 Nov 21;61(22):10276-10298. doi: 10.1021/acs.jmedchem.8b01467. Epub 2018 Oct 31. J Med Chem. 2018. PMID: 30339387
Biphenylsulfonyl-thiophene-carboxamidine inhibitors of the complement component C1s.
Travins JM, Ali F, Huang H, Ballentine SK, Khalil E, Hufnagel HR, Pan W, Gushue J, Leonard K, Bone RF, Soll RM, DesJarlais RL, Crysler CS, Ninan N, Kirkpatrick J, Cummings MD, Huebert N, Molloy CJ, Gaul M, Tomczuk BE, Subasinghe NL. Travins JM, et al. Among authors: desjarlais rl. Bioorg Med Chem Lett. 2008 Mar 1;18(5):1603-6. doi: 10.1016/j.bmcl.2008.01.064. Epub 2008 Jan 19. Bioorg Med Chem Lett. 2008. PMID: 18242991
Enhancement of kinase selectivity in a potent class of arylamide FMS inhibitors.
Illig CR, Manthey CL, Meegalla SK, Wall MJ, Chen J, Wilson KJ, DesJarlais RL, Ballentine SK, Schubert C, Crysler CS, Chen Y, Molloy CJ, Chaikin MA, Donatelli RR, Yurkow E, Zhou Z, Player MR, Tomczuk BE. Illig CR, et al. Among authors: desjarlais rl. Bioorg Med Chem Lett. 2013 Dec 1;23(23):6363-9. doi: 10.1016/j.bmcl.2013.09.061. Epub 2013 Oct 1. Bioorg Med Chem Lett. 2013. PMID: 24138939
Discovery of novel FMS kinase inhibitors as anti-inflammatory agents.
Illig CR, Chen J, Wall MJ, Wilson KJ, Ballentine SK, Rudolph MJ, DesJarlais RL, Chen Y, Schubert C, Petrounia I, Crysler CS, Molloy CJ, Chaikin MA, Manthey CL, Player MR, Tomczuk BE, Meegalla SK. Illig CR, et al. Among authors: desjarlais rl. Bioorg Med Chem Lett. 2008 Mar 1;18(5):1642-8. doi: 10.1016/j.bmcl.2008.01.059. Epub 2008 Jan 19. Bioorg Med Chem Lett. 2008. PMID: 18242992
Structure-based optimization of a potent class of arylamide FMS inhibitors.
Meegalla SK, Wall MJ, Chen J, Wilson KJ, Ballentine SK, Desjarlais RL, Schubert C, Crysler CS, Chen Y, Molloy CJ, Chaikin MA, Manthey CL, Player MR, Tomczuk BE, Illig CR. Meegalla SK, et al. Among authors: desjarlais rl. Bioorg Med Chem Lett. 2008 Jun 15;18(12):3632-7. doi: 10.1016/j.bmcl.2008.04.059. Epub 2008 Apr 26. Bioorg Med Chem Lett. 2008. PMID: 18495479
Reducing ion channel activity in a series of 4-heterocyclic arylamide FMS inhibitors.
Wilson KJ, Illig CR, Chen J, Wall MJ, Ballentine SK, DesJarlais RL, Chen Y, Schubert C, Donatelli R, Petrounia I, Crysler CS, Molloy CJ, Chaikin MA, Manthey CL, Player MR, Tomczuk BE, Meegalla SK. Wilson KJ, et al. Among authors: desjarlais rl. Bioorg Med Chem Lett. 2010 Jul 1;20(13):3925-9. doi: 10.1016/j.bmcl.2010.05.013. Epub 2010 May 12. Bioorg Med Chem Lett. 2010. PMID: 20570147
64 results